Abstract: A heteroaryl[4,3-c]pyrimidin-5-amine derivative, a preparation method therefor, and medical uses thereof are provided. Specifically, a heteroaryl[4,3-c]pyrimidin-5-amine derivative of formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and uses thereof as therapeutic agents are provided. In particular, the provided compounds can be used as A2a receptor antagonists and for treatment of conditions or symptoms that are ameliorated by inhibiting the A2a receptor. The various substituent groups in the formula (I) have the meanings as described in the specification.
Abstract: The present invention relates to a method for preparing a pyrimidone heteroaryl derivative and an intermediate of the pyrimidone heteroaryl derivative. Specifically, the pyrimidone heteroaryl derivative of the formula is prepared by changing a starting raw material and an intermediate.
Abstract: A solid dispersion, a method for preparing same, and a solid preparation including the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynylacyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazine-7-one or a pharmaceutically acceptable salt thereof, and a carrier material. The carrier material is selected from hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate.
Abstract: Provided are a crystal form of an oxopicolinamide derivative and a preparation method therefor. In particular, provided are crystal forms A, B, C, D, E, and F of a compound as shown in formula (I) and a preparation method therefor. Crystal forms A, B, C, D, E, and F of the compound of formula (I) obtained in the present disclosure have good crystal stability and chemical stability, and can be better used in clinical treatment.
Type:
Grant
Filed:
February 26, 2019
Date of Patent:
April 12, 2022
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Junran Yang, Lin Wang, Qiyun Shao, Zhenxing Du, Likun Wang
Abstract: The present invention provides a crystal form of a 1,2,3-triazolo[1,5-a]pyrazines derivative and a preparation method for the crystal form. Specifically, the present invention provides a crystal form of a compound (S)-N5-(3,4-difluorophenyl)-6-methyl-N3-((R)-1,1,1-trifluoropropan-2-yl)-6,7-dihydro-[1,2,3]triazolo[1,5-c]pyrazine-3,5(4H)-dimethylformamide and a preparation method for the crystal form. The prepared crystal form has good stability and clinical application value.
Abstract: The present disclosure relates to a pharmaceutical composition, which comprises an IL-15 protein complex and a citrate buffer solution. In addition, the pharmaceutical composition may also comprise a sugar and a non-ionic surfactant. The pharmaceutical composition in the present disclosure demonstrates a high degree of stability even after being stored at 2-8° C. for several months.
Abstract: The present invention provides a fusion protein containing TGF-? receptor and pharmaceutical use thereof. Further, the present invention provides a bifunctional fusion protein comprising the PD-L1 antibody targeting portion and the TGF-?RII extracellular domain, and a pharmaceutical composition comprising the fusion protein containing TGF-? receptor, and the use thereof in the preparation of anti-cancer drug.
Abstract: The present invention relates to a piperazine heteroaryl derivative, a preparation method therefor and the use of same in medicine. In particular, the present invention relates to the piperazine heteroaryl derivative as shown in the general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and the use of same as a capsid protein inhibitor, in particular in the prevention and/or treatment of diseases such as hepatitis B, influenza, herpes, AIDS, etc. The definitions of each group in the general formula (I) are the same as those defined in the description.
Abstract: A pharmaceutical composition for topical administration and a preparation method therefor are described. In particular, a pharmaceutical composition comprising (3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide, or a pharmaceutically acceptable salt thereof, and diethylene glycol monoethyl ether is described.
Abstract: The present invention relates to crystal forms of an oxypyridine amide derivative and a preparation method therefor. In particular, the present invention relates to crystal forms A, B, C, D, E and F of a compound represented by formula (I) and a preparation method therefor. The crystal forms of the compound represented by formula (I) as described in the present invention have good crystal form stability and may be better for clinical use.
Abstract: A method for preparing a tyrosine kinase inhibitor and a derivative thereof are described. In particular, the present method has a short synthesis route, low costs, easy operation, and is suitable for large-scale production.
Type:
Grant
Filed:
August 28, 2020
Date of Patent:
December 14, 2021
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Guaili Wu, Quanliang Zhang, Yongxing Cao
Abstract: A crystal form of PARP-1 inhibitor and a preparation method therefor are described. Specifically, a crystal form A of 4-[[3-[[2-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[1,5-?]pyrazine-7-yl]carbonyl]-4-fluorophenyl]methyl-1(2H)-phthalazinone (formula I) and a preparation method therefor are described.
Type:
Grant
Filed:
August 23, 2018
Date of Patent:
November 23, 2021
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Wenhai Li, Quanliang Zhang, Zhenjun Qiu, Zhengming Li
Abstract: A salt of a phenylpropionamide derivative and a preparation method therefor is described. Specifically, the salt of the compound of formula (I) has good stability, and can be better used in clinical treatment. The process for preparing the salt of the compound of formula (I) of the present invention is simple and easy to operate.
Abstract: Provided are a crystal form of a maleate of a tyrosine kinase inhibitor and a preparation method therefor. Specifically, provided are I crystal form, a II crystal form, a III crystal form, a IV crystal form and a V crystal form of the compound as shown in formula (I) and a preparation method therefor. The new crystal form has a good stability, thereby making same better to use in clinical treatments.
Type:
Application
Filed:
October 21, 2019
Publication date:
November 18, 2021
Applicant:
JIANGSU HENGRUI MEDICINE CO., LTD.
Inventors:
Zhenjun QIU, Quanliang ZHANG, Yanli WEI, Yongxing CAO, Junran YANG, Yahui MA, Zhenxing DU, Jie WANG
Abstract: The present invention relates to a new crystalline form of obeticholic acid and a preparation method therefor. In particular, the present invention relates to crystal form E of obeticholic acid and a preparation method therefor. The crystalline form is very stable, and the solvent residue is low, and the crystalline form is suitable for industrial production.
Abstract: Provided are a LAG-3 antibody, an antigen-binding fragment thereof, and a pharmaceutical application thereof. Further, provided are a chimeric antibody comprising a CDR of the LAG-3 antibody, a humanized antibody, a pharmaceutical composition comprising the LAG-3 antibody and the antigen-binding fragment thereof, and an application of the pharmaceutical composition as an antineoplastic drug. Particularly, provided is an application of a humanized LAG-3 antibody in preparation of drugs for treatment of diseases involving immune cells.
Abstract: This application describes a crystal of a benzofuran derivative free base and a preparation method. Specifically, this application describes crystal A, crystal B, crystal C, and crystal D of N-((4,6-dimethyl-2-carbonyl-1,2-dihydropyridin-3-yl)methyl)-5-ethyl-6-(ethyl(tetrahydro-2H-pyran)4-yl)amino)-2-(piperidin-1-ylmethyl)benzofuran-4-carboxamide and a preparation method for the crystals. The crystals of the compound of formula (I) have great crystal stability and provides improved uses in clinical treatment.
Type:
Grant
Filed:
May 17, 2018
Date of Patent:
October 26, 2021
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Likun Wang, Zhenxing Du, Qiyun Shao, Chao Xu
Abstract: Disclosed are a pyrazolo-heteroaryl derivative, a preparation method and medical use thereof. In particular, this invention relates to a new pyrazolo-heteroaryl derivative as shown in the general formula (I), a preparation method thereof and a pharmaceutical composition containing the derivative and the use thereof as a therapeutic agent, in particular as a TLR7 agonist, wherein each substituent in the general formula (I) is defined in the description.
Abstract: Disclosed is a pharmaceutical composition containing a bicyclo-substituted pyrazolone azo derivative or a salt thereof and a preparation method thereof. In particular, the pharmaceutical composition disclosed in the present invention contains (Z)-5-(2-hydroxyl-3-(2-(3-methyl-5-oxo-1-(5,6,7,8-tetrahydronaphthalene-2-yl)-1H-pyrazol-4(5H)-ylidene)hydrazino)phenyl)furan-2-carboxylic acid or a pharmaceutically acceptable salt thereof, and at least one filler optionally selected from cellulose, microcrystalline cellulose, lactose and starch. The composition has a good stability, dissolution rate and bioavailability, and the preparation process is simple, economical and quick.